Making Targeted Therapy Compatible with Checkpoint Immunotherapy

Abstract

Immune checkpoint blockades induced by antibodies are revolutionizing cancer therapy. Combinations of checkpoint immunotherapies with kinase inhibitors (KIs) are being clinically evaluated as oncogenic mutations arise. Off-target KI cross-reactivity will often compromise synergistic efficacy, with KIs suppressing T-cell functionalities that checkpoint blockers are purportedly boosting. This incompatibility may be removed through molecular optimization.